54796-51-9Relevant academic research and scientific papers
Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase
Hawker, Dustin D.,Silverman, Richard B.
, p. 5763 - 5773 (2012/11/06)
Two principal neurotransmitters are involved in the regulation of mammalian neuronal activity, namely, γ-aminobutyric acid (GABA), an inhibitory neurotransmitter, and l-glutamic acid, an excitatory neurotransmitter. Low GABA levels in the brain have been implicated in epilepsy and several other neurological diseases. Because of GABA's poor ability to cross the blood-brain barrier (BBB), a successful strategy to raise brain GABA concentrations is the use of a compound that does cross the BBB and inhibits or inactivates GABA aminotransferase (GABA-AT), the enzyme responsible for GABA catabolism. Vigabatrin, a mechanism-based inactivator of GABA-AT, is currently a successful therapeutic for epilepsy, but has harmful side effects, leaving a need for improved GABA-AT inactivators. Here, we report the synthesis and evaluation of a series of heteroaromatic GABA analogues as substrates of GABA-AT, which will be used as the basis for the design of novel enzyme inactivators.
Synthesis of N-(Methoxycarbonylthienylmethyl)thioureas and evaluation of their interaction with inducible and neuronal nitric oxide synthase
Suaifan, Ghadeer A.R.Y.,Goodyer, Claire L.M.,Threadgill, Michael D.
experimental part, p. 3121 - 3134 (2010/09/04)
Two isomeric N-(memoxycarbonylmienylmemyl)mioureas were synthesised by a sequence of radical bromination of methylthiophenecarboxylic esters, substitution with trifluoroacetamide anion, deprotection, formation of the corresponding isothiocyanates and addition of ammonia. The interaction of these new thiophene-based thioureas with inducible and neuronal nitric oxide synthase was evaluauted. These novel thienylmethyl- thioureas stimulated the activity of inducible Nitric Oxide Synthase (iNOS).
QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
-
Page/Page column 80, (2008/06/13)
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
QUINOXALINES AS B RAF INHIBITORS
-
Page/Page column 79, (2010/11/08)
The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
TRICYCLIC DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
-
Page 74, (2010/02/10)
The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
Aminomethylthiophene-2-carboxylic acids as dipeptide mimetic in new growth hormone secretagogues
Peschke, Bernd,Madsen, Kjeld,Hansen, Birgit Sehested,Johansen, Nils Langeland
, p. 1969 - 1972 (2007/10/03)
3-Aminomethylbenzoic acid is a well established dipeptide mimetic. Herein, aminomethylthiophene-2-carboxylic acids have been synthesized as analogues of 3-aminomethylbenzoic acid. Their use as a dipeptide-mimetic at the N-terminal of novel growth hormone secretagogues is described.
